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Identification
NameUrofollitropin
Accession NumberDB00094  (BIOD00104, BTD00104)
TypeBiotech
GroupsApproved
Description

Urofollitropin is a purified form of follicle-stimulating hormone (FSH) that is manufactured by extraction from human urine and then purified. It consists of two non-covalently linked, non-identical glycoproteins designated as the alpha- and beta- subunits. The alpha- and beta- subunits have 92 and 111 amino acids. The alpha subunit is glycosylated at Asn 51 and Asn 78 while the beta subunit is glycosylated at Asn 7 and Asn 24. Urofollitropin is important in the development of follicles produced by the ovaries. Given by subcutaneous injection, it is used in combination with human chorionic gonadotropin (hCG) to assist in ovulation and fertility. Urofollitropin may also be used to cause the ovary to produce several follicles, which can then be harvested for use in gamete intrafallopian transfer (GIFT) or in vitro fertilization (IVF).

Protein structureNo structure small
Protein chemical formulaC42H65N11O12S2
Protein average weight980.1620
Sequences
>Alpha chain
APDVQDCPECTLQENPFFSQPGAPILQCMGCCFSRAYPTPLRSKKTMLVQKNVTSESTCC
VAKSYNRVTVMGGFKVENHTACHCSTCYYHKS
>Beta chain
NSCELTNITIAIEKEECRFCISINTTWCAGYCYTRDLVYKDPARPKIQKTCTFKELVYET
VRVPGCAHHADSLYTYPVATQCHCGKCDSDSTDCTVRGLGPSYCSFGEMKE
Download FASTA Format
Synonyms
SynonymLanguageCode
Follicle Stimulating HormoneNot AvailableNot Available
Follicle-stimulating hormone beta subunitNot AvailableNot Available
Follitropin beta chain precursorNot AvailableNot Available
FSHNot AvailableNot Available
FSH-BNot AvailableNot Available
FSH-betaNot AvailableNot Available
UrofollitrophinNot AvailableNot Available
SaltsNot Available
Brand names
NameCompany
BravelleFerring Pharmaceuticals Inc.
FertinexSerono S.A.
MetrodinSerum Inst.
Brand mixturesNot Available
Categories
CAS number146479-72-3
Taxonomy
KingdomOrganic Compounds
SuperclassOrganic Acids
ClassCarboxylic Acids and Derivatives
SubclassAmino Acids, Peptides, and Analogues
Direct parentPeptides
Alternative parentsNot Available
SubstituentsNot Available
Classification descriptionNot Available
Pharmacology
IndicationFor treatment of female infertility
PharmacodynamicsUsed for the treatment of female infertility, urofollitropin or follicle stimulating hormone (FSH) stimulates ovarian follicular growth in women who do not have primary ovarian failure. FSH, the active component of urofollitropin is the primary hormone responsible for follicular recruitment and development.
Mechanism of actionFSH binds to the follicle stimulating hormone receptor which is a G-coupled transmembrane receptor. Binding of the FSH to its receptor seems to induce phosphorylation and activation of the PI3K (Phosphatidylinositol-3-kinase) and Akt signaling pathway, which is known to regulate many other metabolic and related survival/maturation functions in cells.
Absorption74%
Volume of distribution

Time to peak in plasma:
IM: 17 hours (single dose), 11 hours (multiple doses)
SubQ: 21 hours (single dose), 10 hours (multiple doses)

Protein bindingNot Available
Metabolism
Route of eliminationVia liver and kidneys
Half lifeCirculation half life of 3-4 hours, elimination half life of 35-40 hours
ClearanceNot Available
ToxicityNot Available
Affected organisms
  • Humans and other mammals
PathwaysNot Available
SNP Mediated EffectsNot Available
SNP Mediated Adverse Drug ReactionsNot Available
Pharmacoeconomics
Manufacturers
  • Serono laboratories inc
  • Ferring pharmaceuticals inc
Packagers
Dosage forms
FormRouteStrength
Powder, for solutionIntramuscular
Prices
Unit descriptionCostUnit
Fertinex 75 unit Solution103.85USDvial
Bravelle 75 unit vial93.85USDvial
DrugBank does not sell nor buy drugs. Pricing information is supplied for informational purposes only.
Patents
CountryPatent NumberApprovedExpires (estimated)
United States57670671995-06-162015-06-16
Properties
Stateliquid
Experimental Properties
PropertyValueSource
melting point55 °CForastieri, H., Ingham, K.C. J. Biol. Chem. 257:7976-7981 (1982)
hydrophobicity-0.330Not Available
isoelectric point7.50Not Available
References
Synthesis ReferenceNot Available
General Reference
  1. Goa KL, Wagstaff AJ: Follitropin alpha in infertility: a review. BioDrugs. 1998 Mar;9(3):235-60. Pubmed
    #Lexicomp. Urofollitropin. N.p., 2014. Web. 11 Nov. 2014. http://online.lexi.com.login.ezproxy.library.ualberta.ca/lco/action/doc/retrieve/docid/patch_f/797#f_pharmacology-and-pharmacokinetics
External Links
ResourceLink
UniProtP01225
GenbankM16647
PharmGKBPA451835
Drug Product Database2268140
RxListhttp://www.rxlist.com/cgi/generic3/urofollitropin.htm
Drugs.comhttp://www.drugs.com/cdi/urofollitropin-purified.html
WikipediaUrofollitropin
ATC CodesG03GA04
AHFS Codes
  • 68:18.00
PDB Entries
FDA labelshow(174 KB)
MSDSNot Available
Interactions
Drug InteractionsSearched, but no interactions found.
Food InteractionsNot Available

Targets

1. Follicle-stimulating hormone receptor

Kind: protein

Organism: Human

Pharmacological action: yes

Actions: agonist

Components

Name UniProt ID Details
Follicle-stimulating hormone receptor P23945 Details

References:

  1. Layman LC: Mutations in the follicle-stimulating hormone-beta (FSH beta) and FSH receptor genes in mice and humans. Semin Reprod Med. 2000;18(1):5-10. Pubmed
  2. Leng N, Dattatreyamurty B, Reichert LE Jr: Identification of amino acid residues 300-315 of the rat FSH receptor as a hormone binding domain: evidence for its interaction with specific regions of FSH beta-subunit. Biochem Biophys Res Commun. 1995 May 16;210(2):392-9. Pubmed
  3. Santa Coloma TA, Dattatreyamurty B, Reichert LE Jr: A synthetic peptide corresponding to human FSH beta-subunit 33-53 binds to FSH receptor, stimulates basal estradiol biosynthesis, and is a partial antagonist of FSH. Biochemistry. 1990 Feb 6;29(5):1194-200. Pubmed
  4. Dattatreyamurty B, Reichert LE Jr: Identification of regions of the follitropin (FSH) beta-subunit that interact with the N-terminus region (residues 9-30) of the FSH receptor. Mol Cell Endocrinol. 1993 May;93(1):39-46. Pubmed
  5. Lindau-Shepard B, Roth KE, Dias JA: Identification of amino acids in the C-terminal region of human follicle-stimulating hormone (FSH) beta-subunit involved in binding to human FSH receptor. Endocrinology. 1994 Sep;135(3):1235-40. Pubmed
  6. Chen X, Ji ZL, Chen YZ: TTD: Therapeutic Target Database. Nucleic Acids Res. 2002 Jan 1;30(1):412-5. Pubmed

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Drug created on June 13, 2005 07:24 / Updated on November 11, 2014 13:44